Mepitiostane

Mepitiostane is an ethylestrenol ether and a synthetic, orally active androgen and anabolic steroid (AAS) that is used in the treatment of breast cancer. It is marketed under the brand name Thioderon. Mepitiostane is a prodrug of ethylestrenol, meaning it is metabolically converted into ethylestrenol within the body. This conversion is necessary for its activity, as ethylestrenol is the active form of the drug.

Medical Uses

Mepitiostane is primarily used in the treatment of breast cancer in women. Its effectiveness in this application is attributed to its ability to reduce estrogen levels in the body, which can help to slow the growth of estrogen-sensitive cancer cells.

Pharmacology

Mechanism of Action

As an androgen and anabolic steroid, mepitiostane's mechanism of action involves its conversion to ethylestrenol, which then exerts anabolic and androgenic effects. These effects are mediated through the activation of the androgen receptor (AR), leading to various physiological and pharmacological outcomes. In the context of breast cancer, the reduction in estrogen levels is a key therapeutic effect.

Pharmacokinetics

Mepitiostane is administered orally. Upon ingestion, it is converted into ethylestrenol, its active metabolite. The pharmacokinetics of mepitiostane, including its absorption, distribution, metabolism, and excretion, are closely tied to those of ethylestrenol.

Adverse Effects

Like other androgens and anabolic steroids, mepitiostane can cause a range of adverse effects. These may include virilization in women, hepatotoxicity, alterations in lipid profiles, and changes in libido. The severity and occurrence of these side effects can vary based on the dosage and duration of treatment.

Contraindications

Mepitiostane is contraindicated in patients with known hypersensitivity to the drug or its components. It is also contraindicated in individuals with prostate cancer, as androgens can accelerate the growth of prostate cancer cells. Pregnant and breastfeeding women should avoid using mepitiostane due to potential risks to the fetus or infant.

See Also

• Anabolic steroid
• Breast cancer
• Androgen receptor

References

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